Brand name
- TRIFLUOPERAZINE®
Drug Class
- Antianxiety
- Antiemetic
- Antipsychotic
Preparations
- Trifluoperazine Hydrochloride Tablets BP 1, 2, 5, 10 and 20 mg
Indications
- Control of excessive anxiety, tension and agitation.
- Treatment or prevention of nausea and vomiting of various causes.
- Management of psychotic disorders (e.g. acute or chronic catatonic, hebephrenic and paranoid schizophrenia; psychosis due to organic brain damage, toxic psychosis, and the manic phase of manic-depressive illness.)
Pharmacology
- Phenothiazines act on the subcortical areas of the CNS which influence the affective functions.
- Antagonist for the postsynaptic mesolimbic dopaminergic D2 receptors in the brain and decreases the release of hypothalamic and hypophyseal hormones.
Metabolism
- Half Life: 24 hours
- Onset of action:
- 5 to 1 hour (following oral administration)
- 10 to 15 minutes (following intramuscular administration)
- 5 to 15 minutes (following intravascular administration)
- Peak of action: 2 hours
- Metabolism: Liver
Dosing
- Adults:
- Mild to moderate symptoms:
- Usual dosage: 1 or 2 mg twice daily
- Moderate to severe symptoms:
- Starting dose: 5 mg orally 2 or 3 times daily
- Usual dose: 15 to 20 mg/day
- Max dose: 80 mg/day
- Mild to moderate symptoms:
- Children: (6 to 12 years of age):
- Behavior Disorders in Children:
- Usual dose is: 1 mg once or twice a day (depends on the child’s bodyweight)
- Psychotic Children: (either hospitalized or under adequate supervision)
- Starting dose: 1 mg once or twice daily (depends on the child’s bodyweight)
- Max dose: 15 mg/day
- Behavior Disorders in Children:
Drug Interactions
- Oral anticoagulants
- Propranolol
- Anticonvulsants (e.g., phenytoin)
- Sedatives
- Narcotics
- Anesthetics
- Tranquilizers
- Alcohol
- Antihypertensive
- Levodopa
- Atropine
- Organophosphate insecticides
- Drugs that prolong Qt interval and torsade de pointes:
- Class ia antiarrhythmic (e.g., quinidine, procainamide, disopyramide)
- Class iii antiarrhythmic (e.g., amiodarone, sotalol, ibutilide)
- Antipsychotics (e.g., chlorpromazine, pimozide, droperidol)
- Antidepressants (e.g., fluoxetine, venlafaxine, tricyclic/tetracyclic antidepressants)
- Opioids (e.g., methadone)
- Macrolide antibiotics and analogues (e.g., erythromycin, clarithromycin)
- Quinolone antibiotics (e.g., moxifloxacin)
- Pentamidine
- Antimalarial
- Azole antifungals (e.g., fluconazole, itraconazole, ketoconazole, voriconazole)
- Domperidone
- Tacrolimus
- 5-ht3 antagonists (e.g., dolasetron, ondansetron)
- Beta-2 adrenoceptor agonists (e.g., salmeterol, formoterol)
- Lithium
- Drugs causing electrolyte alteration
- SSRIs (selective serotonin reuptake inhibitor) antidepressants
Adverse Effects
- Extrapyramidal Symptoms
- Motor Restlessness
- Neuroleptic Malignant Syndrome
- Pseudo-parkinsonism
- Tardive Dyskinesia
- Cardiovascular
- nonspecific ECG changes, reversible Q and T wave distortions, QT Prolongation, hypotension, cardiac arrhythmias including atrioventricular block, paroxysmal tachycardia, ventricular fibrillation and cardiac arrest, Ventricular arrhythmias, and Torsade’s de pointes.
- Haematological
- Blood dyscrasias including pancytopenia, agranulocytosis, thrombocytopenic purpura, leucopoenia, eosinophilia, haemolytic anaemia, aplastic anaemia.
- Other Adverse Reactions
- Skin Reactions, Stimulation, Insomnia, Anorexia, Amenorrhea, Lactation, drowsiness, dizziness, fatigue, blurred vision, seizures, altered CSF proteins, cerebral oedema, prolongation of the action of CNS depressants (opiates, alcohol, barbiturates), autonomic reactions (mouth dryness nasal congestion, headache, nausea, constipation, ileus, impotence, urinary retention, priapism, miosis, and mydriasis), muscular weakness, reactivation of psychotic processes (catatonic-like states), increased aggressiveness, and toxic confusional states
Contraindications
- Hypersensitivity
- Comatose or greatly depressed
- Blood dyscrasias and bone marrow depression
- Liver damage
- Congenital long QT syndrome or with a family history of this syndrome
- Cardiac arrhythmias or Torsade de Pointes.
- Combination with serotonin reuptake inhibitors, such as citalopram.
Pregnancy and Breastfeeding
- Pregnancy: category C
- Lactation: Not recommended in nursing mothers
Precautions
- Increased Mortality in Elderly Patients with Dementia:
- the causes of death appeared to be cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia)
- Body Temperature Regulation:
- Hyperpyrexia might happen with antipsychotic drugs >>> Appropriate care is advised when prescribing Trifluoperazine to patients who will be experiencing conditions which increase core body temperature (e.g., exercising strenuously, exposure to extreme heat, receiving concomitant medication with anticholinergic activity or being subject to dehydration.)
- Potential for Hypotension:
- High risk group: elderly or debilitated patients
- Avoid hypotension by:
- Large doses should be avoided in patients with impaired cardiovascular systems.
- After initial administration, keep patient lying down and observe for at least 0.5 hour.
- If hypotension occurs:
- Place patient in head-low position with legs raised.
- norepinephrine or phenylephrine can be used as vasoconstrictor
- Increase in mental and physical activity:
- In angina patients this effect is not desirable >>> patients with angina pectoris experience increasing their pain while taking trifluoperazine >>> patients should be observed carefully
- Prolongation of QT Interval:
- Caution in patients with cardiovascular disease or family history of QT prolongation.
- Avoid concomitant QT prolonging drugs.
- Caution when administering in patients with risk factors for Torsade de Pointes:
- Female
- Age 65 years or older
- Baseline prolongation of the qt/qtc interval
- Congenital long qt syndromes
- Family history of qt prolongation, or sudden cardiac death at <50 years
- Cardiac disease
- History of arrhythmias
- Electrolyte disturbances
- Bradycardia
- Acute neurological events
- Hepatic dysfunction, renal dysfunction, and phenotypic/genotypic poor metabolizers of drug
- Diabetes mellitus
- Nutritional deficit
- Autonomic neuropathy
- Caution patient about endocrine and Metabolism side effects of trifluoperazine:
- Hyperprolactinaemia: which may cause galactorrhoea, gynecomastia, oligo-menorrhea or amenorrhoea, and erectile dysfunction, hypogonadism which may lead to decreased bone mineral density in both female and male subjects.
- Hyperglycemia: Patients should have baseline and periodic monitoring of blood glucose and body weight.
- Caution patients about Gastrointestinal side effects:
- The antiemetic action of trifluoperazine may mask signs and symptoms of toxicity or over dosage of other drugs
- Might obscure the diagnosis of conditions such as intestinal obstruction, brain tumor and Reye’s syndrome.
- Caution patient about possibility of priapism.
- Caution patient about hematologic problems:
- Blood dyscrasias (agranulocytosis, anemia, leukopenia, neutropenia, pancytopenia, and thrombocytopenia) and jaundice of the cholestatic type might happen >>> hematological monitoring is recommended.
- Venous thromboembolism (VTE):
- All potential risk factors for VTE should be identified and preventative measures undertaken.
- Caution patients about Hepatic/Biliary/Pancreatic:
- Jaundice of the cholestatic type of hepatitis or liver damage might happen in patients receiving trifluoperazine >>> Hepatic and renal function should be checked
- Caution patients about Neurologic side effects:
- Neuroleptic Malignant Syndrome (NMS)
- Tardive Dyskinesia
- Caution in concomitant use with Anticonvulsants:
- Trifluoperazine lower the convulsive threshold >>> it should be used with caution in patients with epilepsy, EEG abnormalities or subcortical brain damage.
- Caution patients about effects on Driving Ability and Use of Machinery:
- Trifluoperazine impair mental and/or physical abilities >>> patients should be cautioned about activities requiring alertness (e.g., operating vehicles or machinery).
- Caution patients about Dependence/Tolerance:
- Sudden discontinuance in long-term psychiatric patients cause temporary symptoms (e.g., nausea and vomiting, dizziness, tremulousness.)
- Caution patients about Ophthalmologic problem:
- Glaucoma: trifluoperazine should be used with caution in patients with glaucoma.
- Retinopathy: Phenothiazines might produce retinopathy, especially with long-term treatment at high dosage.
- Caution patients about reversible skin pigmentation
- Special Populations:
- Pediatrics (under 6 years of age):
- Not recommended in children under the age of 6.
- Geriatrics (≥65 years of age):
- Not recommended in patients 65 years of age or older
- Caution should be exercised with the use of Trifluoperazine in the elderly patient.
- Use in Geriatric Patients with Dementia
- Care should be exercised in treating elderly or debilitated patients.
- Pediatrics (under 6 years of age):
- Monitoring and Laboratory Tests:
- Phenothiazines result in falsely positive or negative pregnancy test results >>> Caution patients about reliability of pregnancy test during usage of trifluoperazine.
Section
This document is prepared by the “Mental Health for All” team. This document is provided for information purposes only and does not necessarily represent endorsement by or an official position of the Essentials of Medicine. Advice on the treatment or care of an individual patient should be obtained through consultation with a physician who has examined that patient or is familiar with that patient’s medical history.